ChemInform Abstract: Synthesis, Antiinflammatory and Ulcerogenicity Studies of Some Substituted Pyrimido[1,6‐a]azepine Derivatives.

El‐Sayed, Nehad A.; Awadallah, Fadi M.; Ibrahim, Nashwa A.; El‐Saadi, Mohammed T.

doi:10.1002/chin.201042222

Cited by 2 publications

(2 citation statements)

References 1 publication

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“…Thus, N-Mannich bases 270 (NR 2 ¼ 1-pyrrolidinyl, 1piperidinyl, 4-morpholinyl) of pyrimido[1,6-a]azepine derivatives ( Fig. 51) had moderate activity (46e58% reduction of edema compared to that recorded for reference drug diclofenac) [421], whereas N-Mannich bases 271 of a tricyclic system derived from pyrimido[1,6-a]azepine ( Fig. 51) were less potent (anti-inflammatory activity of approximately 40% of that of diclofenac) [422].…”

Section: Anti-inflammatory Activitymentioning

confidence: 94%

Mannich bases in medicinal chemistry and drug design

Roman¹

2015

European Journal of Medicinal Chemistry

257

110

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The biological activity of Mannich bases, a structurally heterogeneous class of chemical compounds that are generated from various substrates through the introduction of an aminomethyl function by means of the Mannich reaction, is surveyed, with emphasis on the relationship between structure and biological activity. The review covers extensively the literature reports that have disclosed Mannich bases as anticancer and cytotoxic agents, or compounds with potential antibacterial and antifungal activity in the last decade. The most relevant studies on the activity of Mannich bases as antimycobacterial agents, antimalarials, or antiviral candidates have been included as well. The review contains also a thorough coverage of anticonvulsant, anti-inflammatory, analgesic and antioxidant activities of Mannich bases. In addition, several minor biological activities of Mannich bases, such as their ability to regulate blood pressure or inhibit platelet aggregation, their antiparasitic and anti-ulcer effects, as well as their use as agents for the treatment of mental disorders have been presented. The review gives in the end a brief overview of the potential of Mannich bases as inhibitors of various enzymes or ligands for several receptors.

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Section: Anti-inflammatory Activitymentioning

confidence: 94%

Mannich bases in medicinal chemistry and drug design

Roman¹

2015

European Journal of Medicinal Chemistry

257

110

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“…A great deal of literature has been found on Schiff bases revealing their important biological activities and a wide range of significant practical applications. Some of their prominent biological activities include antibacterial [20], antifungal [21], antimalarial [22], antiviral [23], inter alia, antitumor [24], herbicidal [25], antioxidant [26], anticonvulsant [27], anti-inflammatory [28], antiproliferative [29], anti HIV [30], antiglycation [31] and lipid lowering [32] properties. Our research group is focused on development of lead molecules through green approach.…”

Section: Introductionmentioning

confidence: 99%

Conventional Versus Microwave Assisted Synthesis, Molecular Docking Studies and In Vitro Evaluation of Benzohydrazide Derivatives as New Acetylcholinesterase and Butyrylcholinesterase Inhibitors

Ali¹,

Rahman²,

Ateeq³

et al. 2016

Med chem (Los Angeles)

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In the course of studies directed towards the synthesis of novel AChE and BChE inhibitors, for the treatment of Alzheimer disease, we focused on the conventional versus microwave assisted synthesis of seventeen benzohydrazide derivatives and tested their ability as AChE and BChE inhibitors. These derivatives were characterized by FT-IR, 1 H-NMR, 13 C-NMR and EI-MS. Seventeen derivatives exhibited varied acetylcholinesterase inhibition with IC 50 values ranging between 72.04 ± 1.12 to 1320.65 ± 0.95 μM as well as butyrylcholinesterase activity with IC 50 values ranging between 3.04 ± 1.48-1876.17 ± 0.95 μM as compared with standard eserine (IC 50 =0.85 ± 0.0001 μM). Only two analogs 3k and 3o exhibited moderate acetylcholinesterase inhibitor potential with IC 50 values 72.04 ± 1.12 and 94.06 ± 1.17 μM respectively. Five analogs 3d, 3h, 3q, 3o and 3l exhibited good potent butyrylcholinesterase inhibitory potential with IC 50 values 3.04 ± 1.48, 9.01 ± 0.58, 15.12 ± 0.66, 45.00 ± 0.99 and 50.19 ± 0.62 μM respectively. Molecular docking studies were carried out in order to find out the binding affinity of benzohydrazide derivatives with the enzyme.

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ChemInform Abstract: Synthesis, Antiinflammatory and Ulcerogenicity Studies of Some Substituted Pyrimido[1,6‐a]azepine Derivatives.

Cited by 2 publications

References 1 publication

Mannich bases in medicinal chemistry and drug design

Mannich bases in medicinal chemistry and drug design

Conventional Versus Microwave Assisted Synthesis, Molecular Docking Studies and In Vitro Evaluation of Benzohydrazide Derivatives as New Acetylcholinesterase and Butyrylcholinesterase Inhibitors

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